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Slow-releasing microball with nimoldipine and its preparing method

A nimodipine-loaded, slow-release microsphere technology, applied in the direction of drug combinations, pharmaceutical formulas, medical preparations of non-active ingredients, etc., to achieve the effects of reducing clogging, low production costs, and stable operation

Inactive Publication Date: 2004-12-15
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, it is mainly used as a primary food raw material at home and abroad, and there are few studies on it as a drug carrier.

Method used

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  • Slow-releasing microball with nimoldipine and its preparing method
  • Slow-releasing microball with nimoldipine and its preparing method
  • Slow-releasing microball with nimoldipine and its preparing method

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0019] 2g of sodium alginate and 0.5g of konjac glucomannan were dissolved in 100ml of deionized water, and 2.2g of nimodipine solid dispersion was added. The weight ratio of nimodipine to 6,000 polyethylene glycol in the solid dispersion was 1: 1. Prepare a konjac glucomannan-sodium alginate mixed solution containing nimodipine solid dispersion. Using capillary crushing method, vibration frequency is 50Hz, flow rate is 138cm / s, the above mixed solution is dropped into CaCl in the form of tiny droplets 2 The concentration is 0.2M, the concentration of chitosan is 0.25% (w / v), and the molecular weight of chitosan is 8.55×10 6 In the chitosan calcium chloride solution, gel for 30 minutes, filter and wash, and dry at 50°C to obtain nimodipine sustained-release microspheres with higher strength and good controlled release properties ( figure 1 ). The average particle size of the microspheres is 0.91mm, the particle size deviation is 10.7%, and the sphericity is good.

example 2

[0021] 2g of sodium alginate and 0.5g of konjac glucomannan were dissolved in 100ml of deionized water, and 2.2g of nimodipine solid dispersion was added. The weight ratio of nimodipine to 6,000 polyethylene glycol in the solid dispersion was 1: 1. Or add 1.1 g of nimodipine plain medicine to the above mixed sol to prepare a konjac glucomannan-sodium alginate mixed solution containing nimodipine solid dispersion or nimodipine plain medicine. According to Example 1, the capillary crushing method was used to prepare sustained-release microspheres containing solid dispersion of nimodipine and nimodipine. After treatment in simulated gastric juice for 4 hours, the gastric juice release rate of the microspheres containing nimodipine and nimodipine solid dispersion were 3.75% and 4.56%, respectively. The microspheres are placed in the simulated intestinal fluid again, and the release of the drug can be seen figure 2 . figure 2 It can be seen that the release rate of the microspheres l...

example 3

[0023] 2g of sodium alginate and 0, 0.25, 0.375, 0.5g of konjac glucomannan were dissolved in 100ml of deionized water, and 2.2g of nimodipine solid dispersion was added respectively. The solid dispersion of nimodipine and the molecular weight of 6000 The weight ratio of polyethylene glycol is 1:1, and nimodipine solid dispersion-konjac glucomannan-sodium alginate mixed solutions with different contents of konjac glucomannan are prepared. According to Example 1, the capillary crushing method was used to prepare drug-loaded konjac glucomannan-calcium alginate-chitosan microspheres with different contents of konjac glucomannan. After 4 hours of treatment in simulated gastric juice, the gastric juice release rate of the above microspheres was all lower than 5%. The particles are again placed in the simulated intestinal fluid, and the release of the drug can be seen image 3 . by image 3 It can be seen that the microspheres containing a higher concentration of konjac glucomannan have...

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Abstract

The slow releasing microballoon with nimoldipine is in single nuclear structure or in core-shell structure. The core material consists of dispersed solid nimoldipine and konjaku glucomannan-calcium alginate; and the shell material is chitosan-calcium alginate polyelectrolyte film. The preparation process includes capillary crushing method to drop the mixed hydrosol of dispersed solid nimoldipine and konjaku glucomannan-calcium alginate into the water solution of CaCl2 or chitosan-CaCl2; water washing and drying the microspherical matter to obtain konjaku glucomannan-calcium alginate or konjaku glucomannan-calcium alginate-chitosan microballoon with medicine. The present invention has the advantages of raised bioavailability and slow release effect of nimoldipine, easy control of medicine release, simple technological process, low production cost and easy scale production.

Description

Technical field [0001] The invention relates to a sustained-release microsphere loaded with nimodipine medicine, which belongs to the improvement of oral nimodipine preparation dosage form. Background technique [0002] Nimodipine (Nimodipine, abbreviated as NMP) is a second-generation pyridine calcium antagonist that preferentially acts on small arteries and selectively acts on cerebral blood vessels. It is mainly used for the treatment of ischemic cerebrovascular disease, migraine, sudden deafness, senile dementia, submarine hemorrhage and hypertension (especially essential hypertension) and other diseases. It has achieved good results It also has the effect of protecting or promoting memory. However, the drug has low solubility and low bioavailability of oral tablets, which is only 3%-28% of intravenous injection. Ordinary tablets need to be taken 3 to 4 times a day. Not only do they take a lot of times, but also the "peak-to-valley" effect of blood concentration is obvious. I...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/4422A61K47/36A61P9/12
Inventor 何明霞王康何志敏
Owner TIANJIN UNIV
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